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- 详细信息
- 文献和实验
- 技术资料
- 库存：
22
- 英文名：
BMS-626529
- CAS号：
701213-36-7
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
10mg 5mg 2mg 50mg
商品属性：
产品描述：
分子式:C24H23N7O4
分子量:473.48
溶解度:≥ 1.48 mg/mL in DMSO, <2.42 mg/mL in EtOH, <2.39 mg/mL in H2O
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
EC50<10 nM against the vast majority of viral isolatesHIV-1 attachment inhibitors represent a new class of entry inhibitors that prevent the initial interaction between virus and host cell by binding to the viral envelope protein gp120 and blocking attachment of the virus to the CD4 receptor on CD4+ T-cells. BMS-626529 is a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T-cells.In vitro: The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. BMS-626529 had half-maximal effective concentration values of <10 nM against the vast majority of viral isolates; however, susceptibility varied by > 6 log10, with half-maximal effective concentration values in the low pM range against the most susceptible viruses. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life [1].In vivo: No animal in-vivo data available currentlyClinical trial: BMS-663068 is a prodrug of the small-molecule inhibitor BMS-626529. The maximum median decreased in plasma HIV-1 RNA load from baseline ranged from 1.21 to 1.73 log10 copies/mL. Plasma concentrations of BMS-626529 were not associated with an antiviral response, while low baseline inhibitory concentrations and the minimum and average steady-state BMS-626529 plasma concentrations, when adjusted by the baseline protein binding–adjusted 90% inhibitory concentration, were linked with antiviral response. BMS-663068 was generally well tolerated [2].References:[1] Nowicka-Sans B, Gong YF, McAuliffe B, Dicker I, Ho HT, Zhou N, Eggers B, Lin PF, Ray N, Wind-Rotolo M, Zhu L, Majumdar A, Stock D, Lataillade M, Hanna GJ, Matiskella JD, Ueda Y, Wang T, Kadow JF, Meanwell NA, Krystal M. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrob Agents Chemother. 2012;56(7):3498-507.[2] Nettles RE, Schürmann D, Zhu L, Stonier M, Huang SP, Chang I, Chien C, Krystal M, Wind-Rotolo M, Ray N, Hanna GJ, Bertz R, Grasela D. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012;206(7):1002-11.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
公司正在出售的产品：
| 货号 | CS-01Y63951 | 规格 | 10mg 5mg 2mg 50mg |
| CAS号 | 701213-36-7 | 分子量 | 473.48 |
| 含量 | >98.00% | 别名 | BMS 626529;BMS626529 |
| 分子式 | C24H23N7O4 | 化学名 | 1-(4-benzoylpiperazin-1-yl)-2-[4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]ethane-1,2-dione |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C24H23N7O4
分子量:473.48
溶解度:≥ 1.48 mg/mL in DMSO, <2.42 mg/mL in EtOH, <2.39 mg/mL in H2O
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
EC50<10 nM against the vast majority of viral isolatesHIV-1 attachment inhibitors represent a new class of entry inhibitors that prevent the initial interaction between virus and host cell by binding to the viral envelope protein gp120 and blocking attachment of the virus to the CD4 receptor on CD4+ T-cells. BMS-626529 is a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T-cells.In vitro: The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. BMS-626529 had half-maximal effective concentration values of <10 nM against the vast majority of viral isolates; however, susceptibility varied by > 6 log10, with half-maximal effective concentration values in the low pM range against the most susceptible viruses. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life [1].In vivo: No animal in-vivo data available currentlyClinical trial: BMS-663068 is a prodrug of the small-molecule inhibitor BMS-626529. The maximum median decreased in plasma HIV-1 RNA load from baseline ranged from 1.21 to 1.73 log10 copies/mL. Plasma concentrations of BMS-626529 were not associated with an antiviral response, while low baseline inhibitory concentrations and the minimum and average steady-state BMS-626529 plasma concentrations, when adjusted by the baseline protein binding–adjusted 90% inhibitory concentration, were linked with antiviral response. BMS-663068 was generally well tolerated [2].References:[1] Nowicka-Sans B, Gong YF, McAuliffe B, Dicker I, Ho HT, Zhou N, Eggers B, Lin PF, Ray N, Wind-Rotolo M, Zhu L, Majumdar A, Stock D, Lataillade M, Hanna GJ, Matiskella JD, Ueda Y, Wang T, Kadow JF, Meanwell NA, Krystal M. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrob Agents Chemother. 2012;56(7):3498-507.[2] Nettles RE, Schürmann D, Zhu L, Stonier M, Huang SP, Chang I, Chien C, Krystal M, Wind-Rotolo M, Ray N, Hanna GJ, Bertz R, Grasela D. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012;206(7):1002-11.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
公司正在出售的产品：
| Boc-Phg-OH | (Des-Pyr¹,Des-Gly¹⁰,D-Leu⁶,Pro-NHEt⁹)-LHRH |
| (Des-Ser³)-ACTH (1-24) (human, bovine, rat) | CRP 猪C反应蛋白ELISA检测试剂盒 |
| (Des-Thr⁵)-Glucagon | HSP-20 猪热休克蛋白20ELISA检测试剂盒 |
| (Des-Thr⁷)-Glucagon | HSP-70 猪热休克蛋白70ELISA检测试剂盒 |
| (Des-Tyr¹)-Leu-Enkephalin | HSP-40 猪热休克蛋白40ELISA检测试剂盒 |
| (Des-Tyr¹)-Met-Enkephalin | HSP-90 猪热休克蛋白90ELISA检测试剂盒 |
| (D-His(Bzl)⁶)-LHRH (1-7) (free acid) | AChRab 猪乙酰胆碱受抗ELISA检测试剂盒 |
| (D-His¹)-Exenatide | HYD 猪氢化可的松ELISA检测试剂盒 |
| (D-His²)-LHRH | sP-Selectin 猪可溶性P选择素ELISA检测试剂盒 |
| (D-His²,D-Ser(tBu)⁶,Azagly¹⁰)-LHRH | MBP 猪髓磷脂碱性蛋白ELISA检测试剂盒 |
| (D-His²,D-Trp⁶)-LHRH | GHRP 猪生长激素释放多肽ELISA检测试剂盒 |
| (Diacetyl)-α-MSH | pERK 猪磷酸化细胞外信号调节激酶ELISA检测试剂盒 |
| (D-Leu⁶)-LHRH (1-8) (free acid) | BMS-626529ACh 猪乙酰胆碱ELISA检测试剂盒 |
| Lalistat 1 | SP-A 猪肺表面活性物质相关蛋白AELISA检测试剂盒 |
| 人Ⅱ型胶原螺旋肽ELISA试剂盒 | ER 猪雌二醇受ELISA检测试剂盒 |
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BMS-626529
￥600 - 3200
